文献类型：期刊文献

中文题名：Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A4 hydrolase aminopeptidase inhibitors

英文题名：Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A_4 hydrolase aminopeptidase inhibitors

作者：Fan Zhang[1];Dang Wu[1];Gao-Lei Wang[1];Shuang Hou[1];Ping Ou-Yang[1];Jin Huang[1];Xiao-Yong Xu[1]

机构：[1]Shanghai Key Laboratory of Chemical Biology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China

年份：2017

卷号：28

期号：5

起止页码：1044

中文期刊名：Chinese Chemical Letters

外文期刊名：中国化学快报（英文版）

收录：CSTPCD;;Scopus;CSCD:【CSCD2017_2018】；PubMed;

基金：financially supported by the National Natural Science Foundation of China(No.21272071);the Fundamental Research Funds for the Central Universities;support from Shanghai Foundation of Science and Technology(No.15431902100)

语种：英文

中文关键词：1;2;3-Benzotriazin-4-one Leukotriene A4 hydrolase Aminopeptidase activity In vitro Aminopeptidase inhibitors

外文关键词：1,2,3-Benzotriazin-4-one Leukotriene A4 hydrolase Aminopeptidase activity In vitro Aminopeptidase inhibitors

摘要：A series of novel 1,2,3-benzotriazin-4-one derivatives were designed,synthesized and their inhibitory activities against leulcotriene A4 hydrolase aminopeptidase in vitro were evaluated.Many compounds showed moderate to good activities at the concentration of 10 μmol/L.Among them,compound Ⅳ-16 exhibited the highest inhibitory activity up to 80.6% with an IC50 of 1.30 ± 0.20 μmol/L The compound Ⅳ-16 was also tested the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA_4H enzyme by molecular docking was studied.It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study.The relationship between structure and inhibitory activity was also preliminarily discussed.
A series of novel 1,2,3-benzotriazin-4-one derivatives were designed,synthesized and their inhibitory activities against leulcotriene A4 hydrolase aminopeptidase in vitro were evaluated.Many compounds showed moderate to good activities at the concentration of 10 μmol/L.Among them,compound Ⅳ-16 exhibited the highest inhibitory activity up to 80.6% with an IC50 of 1.30 ± 0.20 μmol/L The compound Ⅳ-16 was also tested the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA_4H enzyme by molecular docking was studied.It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study.The relationship between structure and inhibitory activity was also preliminarily discussed.